オルリスタット

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H412：長期的影響により水生生物に有害

• 注意書き

  P273：環境への放出を避けること。

オルリスタット 価格

MSDS Information

• (-)-Tetrahydrolipstatin

オルリスタット 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 効能

  抗肥満薬, 膵リパーゼ阻害薬

• 説明

  Orlistat was launched in the UK as Xenical for the long-term treatment of obesity, preferably in conjunction with a moderately reduced calorie diet. Orlistat is a tetrahydro-derivative of the natural hypolipaemic lipstatin (from Streptomyces toxyfncini) and can be obtained either by hydrogenation of lipstatine or by several different synthetic ways involving many steps from ( S ) - rnalic acid. Orlistat is a potent inhibitor of gastrointestinal lipases required for the lipolysis and digestion of dietary fat, in particular of pancreatic lipase ; as a result, it prevents the absorption of about one third of the fat contained in food and acts as an effective weight-reducing therapy. The outcomes of several clinical trials involving thousands of obese patients showed that Orlistat promotes a significant weight loss (often between 5 and 10% after one year) and improves cardiovascular risk factors such as total cholesterol, LDL/HDL ratio, blood glucose levels, insulin, blood pressure. Orlistat has minimal systemic absorption, the majority of the compound itself being recovered in the feces ; it does not affect other gastrointestinal processes, or the absorption of other rnacronutrients such as carbohydrates and proteins.

• 化学的特性

  Off-White Solid

• 使用

  Orlistat is an antiobesity agent. Orlistat is an pancreatic lipase inhibitor.

• 一般的な説明

  Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
  Orlistat is a specific lipase inhibitor derived from lipostatin, which is naturally produced by Streptomyces toxytricini. Lipase inhibition induced by orlistat reduces the absorption of dietary fat, thereby contributing to caloric deficit.

• 生物活性

  Hypolipemic pancreatic, gastric and carboxylester lipase inhibitor. Exhibits no activity at phospholipase A 2 , liver esterase, trypsin and chymotrypsin. Inhibits the thioesterase domain of fatty acid synthase, leading to cell cycle arrest at the G 1 /S boundary in vitro . Prevents the absorption of approximately one third of fat from food and exhibits progastrokinetic, antiobesity and antihypercholesterolemic activity in vivo .

• 合成

  Orlistat can be prepared from the natural compound lipstatin or by fully chemical synthetic routes; one route employs lactonization with ZnCl2, (R)-3-(((l2-boraneyl-t)thio)oxy)pentanal (7), and thiopyridyl ketene acetals (8) as starting materials, followed by a Mitsunobu reaction with N-formyl leucine (10) to afford (−)-tetrahydrolipstatin, while first- and second-generation enantioselective syntheses deliver the product during the Mitsunobu coupling and demonstrate the key intermediate 21 on a large scale[1][2]. A formal synthesis of orlistat proceeds through hydrogenation of intermediate 9a under standard conditions to afford hydroxy-β-lactone 6 in nearly quantitative yield[3]. A formal synthesis of orlistat is achieved via cross metathesis with excess n-nonene in the presence of the first-generation Grubbs catalyst[3].
  

オルリスタット 生産企業

Global(822)Suppliers

オルリスタット スペクトルデータ(¹HNMR、MS)

96829-58-2, オルリスタット キーワード